The present invention relates to a novel pharmaceutically active composition of matter comprising as active ingredient acetylsalicylic acid or sodium salicylate. More particularly, the present invention relates to a novel pharmaceutically active, water-soluble composition of matter comprising acetyl salicylic acid or sodium salicylate as active ingredient, said composition being adapted to substantially reduce, or entirely eliminate undesired side-effects encountered with acetylsalicylic acid and with sodium salicylate. The novel composition of matter are readily soluble in water and comprise ingredients adapted to result in a rapid and complete solubilization of the active ingredient, and in a buffering action, the combined effect being the substantial reduction or elimination of undesired side-effects. The novel pharmaceutical compositions are soluble in water, and results in a palatable pleasant drink, very much similar to natural milk, and this is easily administered to children and to other persons like the aged, physically and mentally retarded and the like, who experience difficulties in swallowing pills. Any desired suitable flavouring agent may be added.
The invention further relates to such novel compositions of matter in unit dosage form. Other and further aspects of the present invention will become apparent hereinafter.
Acetylsalicylic acid is probably the most widely used analgesic, antipyretic and antirheumatic compound. Acetylsalicylic acid is considered to be the best pain-killer amongst common drugs, as reported by an investigating team of the Mayo Clinic, U.S.A. (reported in April 1972). Although used in huge quantities, acetylsalicylic acid is known to cause undesired side effects, and especially gastrointestinal disturbances, in a certain percentage of patients. The first evidence that acetylsalicylic acid is not so innocuous as it appeared to be came from English physicians in the late 1930's (Brit.Med.J. (1938), 1143; Lancet (1938), 12222; Lancet (1954) 917; Brit.Med.J. (1943) 768; Brit.Med.J. (1958), 1062; Brit.Med.J. (1955), 1531; Lancet (1958) 920, etc. A large quantity of information on this subject matter is summarized in "Aspirin and Gastric Damage", A. Muir, Scientific Exhibit, A.M.A. Convention, Atlantic City, N.J. June 8-12, 1959. Amongst the most common side effects there may be mentioned gastro-duodenal bleeding, dyspepsia, and erosive gastritis. From the results it can be concluded that aspirin is a potentially dangerous drug, especially in ulcer patients, but also in some eupeptic individuals. Bleeding is commoner in elderly people who have taken the drug in heavy dosage over a considerable period of time. The drug is a potent actual or precipitating cause of gastro-duodenal bleeding. Batterman (New Eng.J.Med. 1958, 258, 213,) deals in detail with the relative merits of aspirin and buffered aspirin (aspirin 300 mg. dihydroxy-aluminum amino-acetate 100 mg., magnesium carbonate 100 mg.) and comes to the conclusion that times required for analgesia and the degree of analgesia were identical. Also, the frequency of gastro-intestinal intolerance were identical for both buffered and unbuffered aspirin. In U.S. Pat. No. 3,608,064 (Lamb) there is described milk-buffered aspirin. Aspirin is used in powdered or granular form and the ratio of aspirin to milk solids exemplified is about 1:1 by weight. No solubilization is resorted to Comparative results with such compositions of matter are presented in the last Table of this specification. Hereinafter results are presented showing the advantages of the novel composition of matter according to the invention compared with aspirin, with buffered aspirin and with aspirin in combination with milk solids only. Many of the buffered aspirins have the added drawback of gradual decomposition, the decomposition products being still less tolerable than acetylsalicylic acid by itself.
The conventional pharmaceutical compositions containing acetylsalicylic acid or sodium salicylate as active ingredient are generally supplied in unit dosage form in the form of tablets. A certain percentage of patients experience difficulties in the swallowing of such tablets. Amongst these are certain physically or mentally retarded persons, such a those suffering from cerebral palsy, CNS-impairment, hydrocephaly, hemiplegia, Downs syndrome and the like. Some of the conventional preparations in tablet form, integrate completely upon swallowing and cause severe local effects on the mucosa of the stomach.
Quite frequently infants and children ingest large quantities of aspirin tablets and severe effects, including a multitude of cases of death, are caused thereby. Statistics on the fatality rate of such ingestion in the United States are quite surprising and show a large number of fatalities per year.